Description: TG 100801 HCl (TG-100801; TG100801), the hydrochloride salt of TG100801,is an ester prodrug of TG-100572 (TG 100572). TG100801 is a novel and potent dual inhibitor of VEGFr2 and the Src family (Src/YES) kinases with the potential to be used for the treatment of AMD (age-related macular degeneration). It can be topically administered, and can inhibit RTK (receptor tyrosine kinases) and Src kinases such as VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, and Yes with IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM, respectively.
References: J Med Chem. 2008 Mar 27;51(6):1546-59.Related CAS #: 867331-82-6 (free base); 1018069-81-2 (HCl)